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PF-04781340

Chemical Structure : PF-04781340

CAS No.: 1648726-56-0

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PF-04781340 (PF 04781340, PF04781340)

Catalog No.: PC-61080Not For Human Use, Lab Use Only.

PF-04781340 is a potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    PF-04781340 is a potent, selective, CNS penetrant 5-HT2C receptor agonist with Ki of 3 nM and EC50 of 9 nM, without significant P-gp efflux liability.
    PF-04781340 displays >150-fold selectivity over 5-HT2B receptors agonism (EC50=1484 nM).
    PF-04781340 exhibits good metabolic stability in human liver microsomes (HLM) and moderate to good passive permeability in RRCK cells.

    Physicochemical Properties

    M.Wt 267.376
    Formula C17H21N3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    3-benzyl-N-methyl-6,7,8,9-tetrahydro-5H-pyrido[3,4-d]azepin-1-amine

    References

    1. Dvorak CA, et al. ACS Med Chem Lett. 2015 Jul 20;6(9):1015-8.

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